Chemotherapy may still be an essential component to treat cancer in combination with new targeted
therapies. But chemotherapy needs to get smarter in order to make those combination regimens more effective and
also more tolerable, particularly for an aging population. We describe the first time the synthesis and
pharmacological testing of a fusion molecule comprising of the alkylator bendamustine and the HDAC-inhibitor
vorinostat. The drug was designed to allow for the exploitation of both mechanisms of action simultaneously with
the goal to provide a molecule with superior efficacy over the single agents. The pharmacological testing confirms
the full functional capacity of both moieties and encouraging pharmacological data raises the hope that the drug
may turn out to be a great addition to the armentarium of anticancer agents.
Keywords: Alkylation, apoptosis, bifunctional, checkpoint arrest, DNA repair, fusion molecule, HDAC inhibition.
Rights & PermissionsPrintExport